Biomedical subjects
Publications and source records attributed to S Vega.
As a part of a research program directed to the discovery of novel antidepressant agents, a series of new hetero[2,1]benzothiazepine derivatives was synthesized. Some of these compounds antagonized the ptosis and motor depression induced by tetrabenazine and were also active in the Porsolt forced swimming test.
The sensitivity of one-dimensional dynamic magic-angle spinning (MAS) and off-MAS 2H nuclear magnetic resonance spectra to changes in the parameters of jump-type molecular motions is studied. The Floquet theory approach is used to simulate spectra of spins with I = 1, which are involved in exchange processes in rotating solids. The solution of the Bloch-McConnell equations for rotating samples are derived and some simulated frequency spectra are shown. The dependence of the lineshapes of the center and sidebands of the MAS and off-MAS spectra on the exchange parameters are discussed. Experimental results of 2H spectra of perdeuterated dimethyl sulfone, obtained in the temperature range 20-55 degrees C, are demonstrated. The methyl groups in this molecule undergo pi flips at rates that can be detected by MAS and off-MAS NMR. The shapes of the experimental sidebands are compared with simulated results.
The paper reports the synthesis of a series of 5,6,8,9-tetrahydro-4H, 7H-pyrrolo[1,2-a]cyclopenta[b]thieno-[3,2-f][1,4]diazepines and the results of the study on their CNS activity in mice. The pharmacological properties of a previously prepared series of 5,6,7,8,9,10-hexahydro-benzo-analogs is also described.
A series of aryl and hetarylsulfonylhydrazones of aromatic aldehydes were tested for acute toxicity and anticonvulsant activity in mice. Some of these compounds were effective in the MES, pentetrazol and strychnine tests. Thiophene derivatives were the most active terms of the series.
A new series of 11-substituted 6,11-dihydro-6-methyl-dibenzo[c,f]-[1,2]thiazepine S,S-dioxides was synthesized. Some of the components show significant anticonvulsant activity in the MES, pentetrazol and strychnine tests. The more active compounds are devoid of neurotoxic effects.
As an extension of a previous work, in which a number of 4H-pyrrolo-[1,2-a]thieno[2,3-f][1,4]diazepines were described, a new series of derivatives of the isomeric pyrrolo[1,2-a]thieno[3,2-f]diazepines ring system has been synthesized. The products obtained, together with those reported in the previous paper, were tested for acute toxicity and CNS activity in mice.
A series of 4-phenyl-2-thioxo-benzo[4,5]thieno[2,3-d]pyrimidine derivatives endowed with anti-inflammatory and related pharmacological properties were submitted to a more extensive study to know their exact pharmacological profile and their possible side effects. The studied compounds possess a remarkable analgesic activity, devoid of central effects. They also show an interesting anti-inflammatory profile evidenced by their effectiveness in different experimental models of inflammation. In addition, these compounds exhibit none or very little activity on CNS, scarce toxicity and low gastrointestinal aggressivity.
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The method of synthesis and the pharmacological evaluation of (+/-)-6-trans-8b,9,10,11,12,13-trans-13a-Octahydro-5H-7-thia-12a-azabenzo[f]naphth[1,2,3-c,d] azulene (QM-7184), a thiophene analogue of taclamine, are reported. This new drug shows, at variance with the prototype, a neuroleptic profile in rodents. QM-7184 decreases the spontaneous motor activity, blocks the stereotyped behaviour induced by dopaminergic stimulants and reduces conditioned avoidance responses. In all of these tests, the new drug is less potent than the typical neuroleptics haloperidol or butaclamol. Taclamine does not show, as expected, any neuroleptic activity. Like other neuroleptics, QM-7184 blocks striatal dopaminergic receptors and consequently increases the concentration of homovanillic acid and displaces [3H]spiperone binding, although it is a less potent displacer than haloperidol or butaclamol. QM-7184 shows, however, a high affinity for alpha-noradrenergic receptors, both in the cortex and in the striatum, which is about 20 and 90 times higher than those of haloperidol and butaclamol, respectively. In view of the recently suggested role for norepinephrine in the etiology of schizophrenia, it is speculated that drugs of this type may be of interest in the treatment of psychotic illness.
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